- Oxygen-containing five-membered heterocyclic compound, synthesis method, pharmaceutical composition and application
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The invention discloses an oxygen-containing five-membered heterocyclic compound, a synthesis method, a pharmaceutical composition and application thereof, and belongs to the technical field of medicines and preparation and application thereof. The oxygen-containing five-membered heterocycle has the biological activity of inhibiting the protein tyrosine phosphatase SHP2, can be used as a tool compound for researching the biological function relevance of the protein tyrosine phosphatase SHP2 in the cell signal transduction process, and provides a new means for preventing and treating cancers and metabolic and immune diseases.
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Paragraph 0125; 0145; 0150
(2020/11/10)
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- 3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b
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A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.
- Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Sage, Carleton R.,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Tamura, Susan Y.,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
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p. 6619 - 6622
(2008/04/02)
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- 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b
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1-Substituted benzotriazole carboxylic acids have been identified as the first reported examples of selective small-molecule agonists of the human orphan G-protein-coupled receptor GPR109b (HM74), a low-affinity receptor for the HDL-raising drug niacin. N
- Semple, Graeme,Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Sage, Carleton R.,Tamura, Susan Y.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.
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p. 1227 - 1230
(2007/10/03)
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- BENZOTRIAZOLES AND METHODS OF PROPHYLAXIS OR TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF
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The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR refer
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Page/Page column 47-48
(2008/06/13)
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